Total Flavonoids of Alleviates Irinotecan-Induced Colitis Modification of Gut Microbiota and Fecal Metabolism.

Irinotecan (CPT-11)-induced gastrointestinal toxicity strongly limits its anticancer efficacy. Fisch., especially flavonoids, has strong anti-inflammatory and immunomodulatory activities.

The Effect of Prescription on the Framework of Lipid Matrix and In Vitro Properties.

Purpose: To clarify the inner framework and relative properties in vitro of Lyotropic liquid crystal (LLC) based on various prescriptions by using hydrophilic sinomenine hydrochloride (SH) and lipophilic cinnamaldehyde (CA) as model drugs.

Methods: Phase structures were checked by polarized light microscopy (PLM) and small-angle X-ray scattering (SAXS). Rheological studies and Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR) analysis were carried out to reveal their molecular interactions.

Novel berberine derivatives: Design, synthesis, antimicrobial effects, and molecular docking studies.

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities.

On the Structure and Transdermal Profile of Liquid Crystals Based on Phytantriol.

Background: There has been a growing concern in transdermal drug technology over the past several decades. As a novel transdermal delivery system, Lyotropic liquid crystals (LLC) still face challenges such as drug loading, limited drug permeation and instability of systems. LLC system is so sensitive that a very subtle change in composition may induce a phase transformation or conversion of spatial configuration, and result in a diverse percutaneous delivery subsequently.

Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists.

Aim: Retinoic acid receptor-related orphan nuclear receptors (RORs) are orphan nuclear receptors that show constitutive activity in the absence of ligands. Among 3 subtypes of RORs, RORc is a promising therapeutic target for the treatment of Th17-mediated autoimmune diseases. Here, we report novel RORc inverse agonists discovered through structure-based drug design.

Synthesis and evaluation of benzylisoquinoline derivatives for their inhibition on pancreatic lipase and preadipocyte proliferation.

The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, (1)H NMR and (13)C NMR.

Calycosin-7-O-β-D-glucoside regulates nitric oxide /caveolin-1/matrix metalloproteinases pathway and protects blood-brain barrier integrity in experimental cerebral ischemia-reperfusion injury.

Ethnopharmacology Relevance: Astragali Radix (AR) has been used for thousands years to treat ischemic stroke. Calycosin and its glycoside form calycosin-7-O-β-D-glucoside (CG) are two representative isoflavones in Astragali Radix. However, its neurological effects and related molecular mechanisms are largely unknown.

[Cytotoxic alkaloids from stems of Nelumbo nucifera].

Chemical investigation was carried out to study the alkaloids from stems of Nelumbo nucifera and their cytotoxic activities. The constituents were separated by column chromatography, and their structures were elucidated by spectroscopic data analyses. The isolated compounds were evaluated for their cytotoxic activities by MTr method.

Two new flavone glycosides from the seeds of Impatiens balsamina L.

Two new flavone glycosides were isolated from the seeds of Impatiens balsamina L. and their structures were determined as quercetin-3-O-[α-L-rhamnose-(1 → 2)-β-d-glucopyranosyl]-5-O-β-D-glucopyranoside (1), and quercetin-3-O-[(6'''-O-caffeoyl)-α-L-rhamnose-(1 → 2)-β-D-glucopyranosyl]-5-O-β-D-glucopyranoside (2) on the basis of various spectral and chemical studies.

Four anthraquinones from Hedyotis diffusa.

A new anthraquinone has been isolated from the 95% EtOH extract of Hedyotis diffusa and characterized as 2-hydroxy-3-methoxy-6-methyl-9,10-anthraquinone (1) by extensive spectral analysis. The known compounds isolated for the first time from this plant have been identified as 2-hydroxy-3-methoxy-7-methyl-9,10-anthraquinone (2), 2-hydroxy-6-methylanthraquinone (3), and 1,3-dimethoxy-2-hydroxy-9,10-anthraquinone (4).

[Chemical constituents from Hedyotis diffusa].

Objective: To investigate the chemical constituents from Hedyotis diffusa.

Method: The compounds were isolated and purified by various chromatographic techniques and identified by their physicochemical properties and spectral data.

Result: Eight compounds were isolated and identified as octadecyl (E)-p-coumarate (1), p-E-methoxy-cinnamic acid (2), ferulic acid (3), scopoletin (4), succinic acid (5), aurantiamide acetate (6), rubiadin (7), robustaquinone D (8).

[Studies on chemical constituents in root tuber of Cynanchum auriculatum].

Objective: To study chemical constituents from Cynanchum auriculatum.

Method: The chemical components were isolated and purified by silca gel, sephedex-LH-20 and ODS column chromatography. The chemical structures were elucidated on the basis of physicochemical properties and spectral data.

[A new alkaloid from Opuntia vulgaris].

Aim: To study the chemical constituents of the stems of Opuntia vulgaris Mill(Cactaceae).

Methods: The compounds of Opuntia vulgaris were isolated by chromatography of Amberlite Dowex 50 and silica gel, and identified by means of UV, IR, MS, 1D and 2D NMR.

Results: Three compounds were isolated and identified as: opuntin B(I), 4-hydroxyproline(II) and tyrosine(III).